Literature DB >> 12493545

The automated radiosynthesis of [18F]FP-TZTP.

Dale O Kiesewetter1, Bik-kee Vuong, Michael A Channing.   

Abstract

[(18)F]FP-TZTP (3-(3-(3-[(18)F]fluoropropylthio)-1,2,5-thiadiazol-4-yl)-1,2,5,6-tetrahydro-1-methylpyridine) is a muscarinic ligand that displays in vivo selectivity for the M2 subtype. We have developed a one-step radiosynthesis of [(18)F]FP-TZTP that can be conducted with an automated synthesis unit. A number of hardware and software modifications to a Nuclear Interface C-11 Methylation System provided the equipment for the automated radiosynthesis. The manual synthesis produced [(18)F]FP-TZTP in a radiochemical yield of 23.4% +/- 4.3% (EOS, n = 69) with a specific activity of 4377 +/- 2011 mCi/micromol (EOB, n = 100). The automated synthesis unit provided the product in a radiochemical yield of 18.8% +/- 2.4% (EOS, n = 25) with a specific activity of 4112 +/- 2572 mCi/micromol (EOB, n = 25).

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Year:  2003        PMID: 12493545     DOI: 10.1016/s0969-8051(02)00354-2

Source DB:  PubMed          Journal:  Nucl Med Biol        ISSN: 0969-8051            Impact factor:   2.408


  6 in total

1.  Imaging of the muscarinic acetylcholine neuroreceptor in rats with the M2 selective agonist [18F]FP-TZTP.

Authors:  Laura Ravasi; Joji Tokugawa; Toshiyuki Nakayama; Jurgen Seidel; Louis Sokoloff; William C Eckelman; Dale O Kiesewetter
Journal:  Nucl Med Biol       Date:  2011-08-09       Impact factor: 2.408

2.  Why does the agonist [(18)F]FP-TZTP bind preferentially to the M(2) muscarinic receptor?

Authors:  L Ravasi; D O Kiesewetter; K Shimoji; G Lucignani; W C Eckelman
Journal:  Eur J Nucl Med Mol Imaging       Date:  2005-12-07       Impact factor: 9.236

3.  An automated one-step one-pot [(18)F]FCWAY synthesis: development and minimization of chemical impurities.

Authors:  Bik-Kee Vuong; Dale O Kiesewetter; Lixin Lang; Ying Ma; William C Eckelman; Michael A Channing
Journal:  Nucl Med Biol       Date:  2007-05       Impact factor: 2.408

4.  Genetic variation in cholinergic muscarinic-2 receptor gene modulates M2 receptor binding in vivo and accounts for reduced binding in bipolar disorder.

Authors:  D M Cannon; J K Klaver; S K Gandhi; G Solorio; S A Peck; K Erickson; N Akula; J Savitz; W C Eckelman; M L Furey; B J Sahakian; F J McMahon; W C Drevets
Journal:  Mol Psychiatry       Date:  2010-03-30       Impact factor: 15.992

Review 5.  Applications of LC-MS in PET radioligand development and metabolic elucidation.

Authors:  Ying Ma; Dale O Kiesewetter; Lixin Lang; Dongyu Gu; Xiaoyuan Chen
Journal:  Curr Drug Metab       Date:  2010-07       Impact factor: 3.731

Review 6.  Is There a Role for GPCR Agonist Radiotracers in PET Neuroimaging?

Authors:  Matthieu Colom; Benjamin Vidal; Luc Zimmer
Journal:  Front Mol Neurosci       Date:  2019-10-18       Impact factor: 5.639

  6 in total

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